Indirubin-3'-monoxime, a derivative of a chinese antileukemia medicine, inhibits angiogenesis

Although the antiangiogenic activity of indirubin‐3‐monoxime (I3M), a derivative of a Chinese anti‐leukemia medicine, has been demonstrated using transgenic zebrafish, the detail molecular mechanism has not been elicited. To further establish its role in antiangiogenic activity, we tested its potent...

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Bibliographic Details
Published in:Journal of cellular biochemistry 2011-05, Vol.112 (5), p.1384-1391
Main Authors: Kim, Jin-Kyung, Shin, Eun Kyung, Kang, Young-Hee, Park, Jung Han Yoon
Format: Article
Language:English
Subjects:
angiogenesis
Angiogenesis Inhibitors - pharmacology
Angiogenesis Inhibitors - therapeutic use
Animals
Cell Movement - drug effects
Cell Proliferation - drug effects
Down-Regulation
Drugs, Chinese Herbal - pharmacology
Drugs, Chinese Herbal - therapeutic use
endothelial cell
Endothelium, Vascular - cytology
Endothelium, Vascular - drug effects
Humans
indirubin-3-monoxime
Indoles - pharmacology
Indoles - therapeutic use
Mice
Neovascularization, Pathologic - drug therapy
Oximes - pharmacology
Oximes - therapeutic use
Phosphorylation
Umbilical Veins - cytology
Umbilical Veins - drug effects
vascular endothelial growth factor receptor-2
Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors
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Summary:Although the antiangiogenic activity of indirubin‐3‐monoxime (I3M), a derivative of a Chinese anti‐leukemia medicine, has been demonstrated using transgenic zebrafish, the detail molecular mechanism has not been elicited. To further establish its role in antiangiogenic activity, we tested its potential against human umbilical vein endothelial cells (HUVECs) and the in vivo Matrigel plug model was applied to evaluate new vessel formation. We also investigated the molecular mechanisms of I3M‐induced antiangiogenic effects in HUVECs. We found that I3M significantly inhibited HUVEC proliferation (2.5–20 µM), migration (2.5–20 µM), and tube formation (10–20 µM) in HUVECs. The number of microvessels growing from the aortic rings was suppressed by I3M treatment. Moreover, I3M suppressed neovascularization in Matrigel plugs in mice. The underlying antiangiogenic mechanism of I3M was correlated with down‐regulation of the vascular endothelial growth factor receptor‐2 activation, at least a part. These findings emphasize the potential use of I3M in pathological situations involving stimulated angiogenesis, such as tumor development. J. Cell. Biochem. 112: 1384–1391, 2011. © 2011 Wiley‐Liss, Inc.
ISSN:0730-2312
1097-4644
DOI:10.1002/jcb.23055